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Art. -Nr.: HY-182393

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IGN-2098

IGN-2098 is an orally active, competitive histamine H₂receptor antagonist with a pA₂ value of 7.32. IGN-2098 inhibits basal and stimulated gastric acid secretion. IGN-2098 accelerates ulcer healing, suppresses ulcer edge elevation, and protects gastric and duodenal mucosa from damage. IGN-2098 can be used in research related to gastric ulcers.

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CAS. Nr.: 126869-04-3
Formel: C₂₂H₃₂Cl₂N₄O₂
Molecular Weight:455.42

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

IGN-2098 Chemical Structure

CAS. Nr.: 126869-04-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

H₂ Receptor

7.32 (pA2)

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

IGN-2098 competitively antagonizes histamine H₂ receptors in isolated guinea pig atrial specimens with a pA₂ value of 7.32^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

IGN-2098 (10-30 mg/kg; p.o.; twice daily; 14 days) dose-dependently accelerates the healing of acetic acid-induced gastric ulcers in rats, with 10 mg/kg and 30 mg/kg doses achieving 49.6% and 52.7% healing ratios respectively, and significantly reduces ulcer edge prominence compared to controls^[1].
IGN-2098 (1-60 mg/kg; p.o., s.c., i.d., i.p.; single dose) potently inhibits basal gastric secretion in pylorus-ligated rats across multiple routes, with subcutaneous administration showing the highest potency (ED₅₀ 0.7 mg/kg for acid output inhibition)^[2].
IGN-2098 (0.1-30 mg/kg; s.c.; single dose) potently inhibits histamine-stimulated gastric acid secretion in acute fistula rats, with an ED₅₀ of 0.2 mg/kg^[2].
IGN-2098 (0.3-30 mg/kg; s.c.; single dose) potently inhibits Carbachol (HY-B1208)-stimulated gastric acid secretion in acute fistula rats, with an ED₅₀ of 0.3 mg/kg^[2].
IGN-2098 (1-30 mg/kg; s.c.; single dose) potently inhibits Pentagastrin (HY-A0261)-stimulated gastric acid secretion in acute fistula rats, with an ED₅₀ of 0.1 mg/kg^[2].
IGN-2098 (3-60 mg/kg; s.c.; single dose) inhibits 2-deoxy-D-glucose (HY-13966)-stimulated gastric acid secretion in anesthetized rats, with an ED₅₀ of 42.7 mg/kg^[2].
IGN-2098 (3-60 mg/kg; p.o., s.c.; single dose) inhibits pylorus ligation-induced gastric ulcers in rats, with an ED₅₀ of 29.7 mg/kg^[2].
IGN-2098 (1-60 mg/kg; p.o.; single dose) inhibits water-immersion stress-induced gastric mucosal injury in rats, with an ED₅₀ of 8.4 mg/kg^[2].
IGN-2098 (0.3-3 mg/kg; p.o.; single dose) potently inhibits histamine-induced gastric mucosal injury in rats, with an ED₅₀ of 0.9 mg/kg^[2].
IGN-2098 (3-30 mg/kg; p.o.; single dose) inhibits Indomethacin (HY-14397)-induced gastric mucosal injury in rats, with an ED₅₀ of 5.4 mg/kg^[2].
IGN-2098 (1-30 mg/kg; p.o.; single dose) potently inhibits HCl-Aspirin (HY-14654)-induced gastric mucosal injury in rats, with an ED₅₀ of 1.4 mg/kg, making it 8.1 times more potent than roxatidine^[2].
IGN-2098 (3-60 mg/kg; p.o.; single dose) inhibits HCl-ethanol-induced gastric mucosal injury in rats, with an ED₅₀ of 17.0 mg/kg^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (male, 7 weeks old, gastric ulcer induced by 20% acetic acid injection)^[1]
Dosage:

10 mg/kg; 30 mg/kg
Administration:

p.o.; twice daily; 14 days
Result:

Reduced mean ulcer index to 6.4 mm² and achieved a 49.6% healing ratio at 10 mg/kg, with a significant difference versus control.
Reduced mean ulcer index to 6.0 mm² and achieved a 52.7% healing ratio at 30 mg/kg, with a significant difference versus control.
Significantly reduced prominent ulcer edges versus control at both 10 mg/kg and 30 mg/kg.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

1-60 mg/kg (p.o.); 0.3-30 mg/kg (s.c.); 1-30 mg/kg (i.d.); 1-30 mg/kg (i.p.)
Administration:

p.o.; single dose (0.5, 3, or 9 hours before pylorus ligation); s.c.; single dose (0.5 hours before pylorus ligation); i.d.; single dose (immediately after pylorus ligation); i.p.; single dose (0.5 hours before pylorus ligation)
Result:

Reduced gastric juice volume by 53.1% and acid output by 78.5% at 10 mg/kg p.o.
0.5 hours before ligation, with an ED₅₀of 4.3 mg/kg for acid output inhibition.
Reduced acid output by 71.7% at 10 mg/kg p.o.
3 hours before ligation, and by 88.0% at 30 mg/kg p.o.
3 hours before ligation, with an ED₅₀ of 5.0 mg/kg.
Reduced acid output by 66.5% at 30 mg/kg p.o.
9 hours before ligation, and by 78.8% at 60 mg/kg p.o.
9 hours before ligation, with an ED₅₀ of 16.9 mg/kg.
Reduced acid output by 71.2% at 1 mg/kg s.c., with an ED₅₀ of 0.7 mg/kg.
Reduced acid output by 65.0% at 3 mg/kg i.d., with an ED₅₀ of 1.1 mg/kg.
Reduced acid output by 64.5% at 10 mg/kg i.p., with an ED₅₀ of 3.6 mg/kg.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

0.1-30 mg/kg
Administration:

s.c.; single dose (0.5 hours before first histamine administration)
Result:

Reduced histamine-stimulated acid output by 30.3% at 0.1 mg/kg, 69.3% at 0.3 mg/kg, 73.5% at 1 mg/kg, 89.4% at 3 mg/kg, 92.0% at 10 mg/kg, and 97.5% at 30 mg/kg.
Achieved an ED₅₀ of 0.2 mg/kg for acid output inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

0.3-30 mg/kg
Administration:

s.c.; single dose (0.5 hours before carbachol infusion)
Result:

Reduced carbachol-stimulated acid output by 42.9% at 0.3 mg/kg, 65.5% at 1 mg/kg, 78.1% at 3 mg/kg, 85.6% at 10 mg/kg, and 80.8% at 30 mg/kg.
Achieved an ED₅₀ of 0.3 mg/kg for acid output inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

1-30 mg/kg
Administration:

s.c.; single dose (0.5 hours before pentagastrin infusion)
Result:

Reduced pentagastrin-stimulated acid output by 79.5% at 1 mg/kg, 52.7% at 3 mg/kg, 84.9% at 10 mg/kg, and 98.3% at 30 mg/kg.
Achieved an ED₅₀ of 0.1 mg/kg for acid output inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

3-60 mg/kg
Administration:

s.c.; single dose (0.5 hours after stimulated secretion stabilized)
Result:

Reduced 2-deoxy-D-glucose-stimulated acid output by 65.9% at 60 mg/kg.
Achieved an ED₅₀ of 42.7 mg/kg for acid output inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

3-60 mg/kg
Administration:

p.o.; single dose (30 minutes before ligation); s.c.; single dose (7 hours after ligation)
Result:

Reduced ulcer coefficients by 55.9% at 30 mg/kg, and 61.8% at 60 mg/kg.
Achieved an ED₅₀ of 29.7 mg/kg for ulcer inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

1-60 mg/kg
Administration:

p.o.; single dose (30 minutes before stress exposure)
Result:

Reduced lesion length by 43.1% at 3 mg/kg, 59.1% at 10 mg/kg, 55.8% at 30 mg/kg, and 84.0% at 60 mg/kg.
Achieved an ED₅₀ of 8.4 mg/kg for lesion inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

0.3-3 mg/kg
Administration:

p.o.; single dose (30 minutes before histamine administration)
Result:

Reduced lesion area by 86.7% at 3 mg/kg.
Achieved an ED₅₀ of 0.9 mg/kg for lesion inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

3-30 mg/kg
Administration:

p.o.; single dose (30 minutes before indomethacin administration)
Result:

Reduced lesion length by 52.2% at 10 mg/kg, and 91.8% at 30 mg/kg.
Achieved an ED₅₀ of 5.4 mg/kg for lesion inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

1-30 mg/kg
Administration:

p.o.; single dose (30 minutes before HCl-aspirin administration)
Result:

Reduced lesion length by 78.1% at 3 mg/kg, 90.9% at 10 mg/kg, and 95.0% at 30 mg/kg.
Achieved an ED₅₀ of 1.4 mg/kg for lesion inhibition.

Animal Model:

Sprague-Dawley (male, SPF, 220-270g)^[2]
Dosage:

3-60 mg/kg
Administration:

p.o.; single dose (30 minutes before HCl-ethanol administration)
Result:

Reduced lesion length by 62.0% at 20 mg/kg, 77.3% at 30 mg/kg, and 94.1% at 60 mg/kg.
Achieved an ED₅₀ of 17.0 mg/kg for lesion inhibition.

Chemical Information

CAS. Nr. 126869-04-3
Molecular Weight 455.42
Formel C₂₂H₃₂Cl₂N₄O₂
SMILES

O=C1N=C(NC/C=C/COC2=CC=CC(CN3CCCCC3)=C2)NC(C)=C1C.Cl.Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Uchida M, et al. [Therapeutic effect of IGN-2098, a new antiulcer drug (H2-antagonist), in the ulcer diminishing period against acetic acid-induced gastric ulcer in rats]. Nihon Yakurigaku Zasshi. 1995 Mar;105(3):153-9. Japanese.
[Content Brief]

[2]. Okabe S, et al. [Effects of IGN-2098, a new histamine H2-receptor antagonist, on gastric secretion and gastric and duodenal lesions induced in rats. Comparison with roxatidine]. Nihon Yakurigaku Zasshi. 1992 Mar;99(3):167-80. Japanese.
[Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
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- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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IGN-2098

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

IGN-2098 Related Classifications

HY-182393 Related Classifications